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Claims for Patent: 8,298,554

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Claims for Patent: 8,298,554

Title:Stable pharmaceutical composition and methods of using same
Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases.
Inventor(s): Manku; Mehar (Oxford, GB)
Assignee: Amarin Pharmaceuticals Ireland Limited (Dublin, IE)
Application Number:12/769,885
Patent Claims: 1. A pharmaceutical composition comprising at least 95%, by weight of total fatty acids present, eicosapentaenoic acid or ester thereof enclosed in a capsule shell, wherein: (a) the composition has a baseline peroxide value not greater than 5 meq/kg and upon storage of the composition at 25.degree. C. and 60% RH for a period of 6 months, the composition has a second peroxide value not greater than 8 meq/kg (b) the capsule shell is free of succinated gelatin and comprises a film-forming material, a hygroscopic plasticizer selected from glycerin, sorbitol and alkylene glycols, and a non-hygroscopic plasticizer selected from maltitol, lactitol, xylitol, hydrogenated starch hydrolysate and glucose syrup, wherein the hygroscopic plasticizer and non-hygroscopic plasticizer are present in a weight ratio of about 2:1 to about 6:1, and (c) if the capsule shell comprises glycerin and the film-forming material comprises gelatin, the capsule shell has a gelatin:glycerin weight ratio greater than 5:1.

2. The pharmaceutical composition of claim 1 wherein the eicosapentaenoic acid or ester thereof comprises ethyl eicosapentaenoate.

3. The pharmaceutical composition of claim 2 wherein the composition contains less than about 1%, by weight of total fatty acids present, of any individual fatty acid other than ethyl eicosapentaenoate.

4. The pharmaceutical composition of claim 2 wherein the composition contains less than about 0.5%, by weight of total fatty acids present, of any individual fatty acid other than ethyl eicosapentaenoate.

5. The pharmaceutical composition of claim 2 wherein the composition contains less than about 0.3%, by weight of total fatty acids present, docosahexaenoic acid or derivative thereof, if any.

6. The pharmaceutical composition of claim 5 wherein the composition contains substantially no docosahexaenoic acid or derivative thereof.

7. The pharmaceutical composition of claim 1 wherein the composition comprises about 0.1% to about 1%, by weight, of an antioxidant.

8. The pharmaceutical composition of claim 7 wherein the antioxidant is tocopherol.

9. The pharmaceutical composition of claim 1 wherein upon storage of the composition at 25.degree. C. and 60% RH for a period of 6 months, the composition has a second peroxide value not greater than 7 meq/kg.

10. The pharmaceutical composition of claim 1 wherein upon storage of the composition at 25.degree. C. and 60% RH for a period of 6 months, the composition has a second peroxide value not greater than 6 meq/kg.

11. The pharmaceutical composition of claim 1 wherein upon storage of the composition at 30.degree. C. and 65% RH for a period of 6 months, the composition has a second peroxide value not greater than 12 meq/kg.

12. The pharmaceutical composition of claim 11 wherein upon storage of the composition at 30.degree. C. and 65% RH for a period of 6 months, the composition has a second peroxide value not greater than 10 meq/kg.

13. The pharmaceutical composition of claim 1 wherein upon storage of the composition at 30.degree. C. and 65% RH for a period of 6 months, the composition has a second peroxide value not greater than 10 meq/kg.

14. The pharmaceutical composition of claim 13 wherein upon storage of the composition at 30.degree. C. and 65% RH for a period of 6 months, the composition has a second peroxide value not greater than 6 meq/kg.

15. The pharmaceutical composition of claim 1 wherein the film-forming material comprises gelatin and the capsule shell has a weight ratio of gelatin to glycerol of at least about 5.2:1.

16. The pharmaceutical composition of claim 1 wherein the capsule shell has a hygroscopic plasticizer to non-hygroscopic plasticizer weight ratio of about 3:1 to about 5:1.

17. The pharmaceutical composition of claim 1 wherein the composition has a dissolution profile as measured by rotating dialysis cell method wherein: (1) at least about 20% of the eicosapentaenoic acid or ester thereof is dissolved by 10 minutes; (2) at least about 50% of the eicosapentaenoic acid or ester thereof is dissolved by 30 minutes; (3) at least about 80% of the eicosapentaenoic acid or ester thereof is dissolved by 60 minutes; (4) at least about 95% of the eicosapentaenoic acid or ester thereof is dissolved by 100 minutes.

18. The pharmaceutical composition of claim 17 wherein the composition has a dissolution profile as measured by rotating dialysis cell method wherein: (1) at least about 20% of the eicosapentaenoic acid or ester thereof is dissolved by 10 minutes; (2) at least about 45% of the eicosapentaenoic acid or ester thereof is dissolved by 30 minutes; (3) at least about 80% of the eicosapentaenoic acid or ester thereof is dissolved by 60 minutes; and (4) at least about 95% of the eicosapentaenoic acid or ester thereof is dissolved by 100 minutes.

19. The pharmaceutical composition of claim 1 wherein upon administration of said composition to a human subject, the subject achieves an eicosapentaenoic acid T.sub.max within 5.8 hours of said administration.

20. A pharmaceutical composition comprising at least about 95%, by weight of total fatty acids present, ethyl eicosapentaenoate enclosed in a capsule shell, wherein the composition has a baseline peroxide value not greater than 5 meq/kg and upon storage of the composition at 30.degree. C. and 65% RH for a period of 6 months, the composition has a second peroxide value not greater than 5 meq/kg wherein the capsule shell comprises a film-forming material free of chemically modified gelatin, a hygroscopic plasticizer selected from glycerol, sorbitol and alkylene glycols, and a non-hygroscopic plasticizer selected from maltitol, lactitol, xylitol, hydrogenated starch hydrolysate and glucose syrup, the capsule shell having a weight ratio of hygroscopic plasticizer to non-hygroscopic plasticizer of about 2:1 to about 6:1, and wherein if the capsule shell comprises glycerol and the film-forming material comprises gelatin, the capsule shell has a gelatin:glycerol weight ratio greater than 5:1.

21. The pharmaceutical composition of claim 20 wherein the hygroscopic plasticizer comprises glycerol.

22. The pharmaceutical composition of claim 21 wherein the capsule shell has a weight ratio of gelatin to glycerol of at least about 5.2:1.

23. The pharmaceutical composition of claim 22 wherein the non-hygroscopic plasticizer comprises maltitol.

24. The pharmaceutical composition of claim 20 wherein the capsule shell has a hygroscopic plasticizer to non-hygroscopic plasticizer weight ratio of about 3:1 to about 5:1.

25. A pharmaceutical composition comprising at least about 95%, by weight of total fatty acids present, ethyl eicosapentaenoate encapsulated in a capsule shell comprising gelatin, a hygroscopic plasticizer selected from glycerol, sorbitol and alkylene glycols, and a non-hygroscopic plasticizer selected from maltitol, lactitol, xylitol, hydrogenated starch hydrolysate and glucose syrup, wherein the capsule shell has a weight ratio of gelatin to total plasticizer of about 1.75:1 to about 5:1 and a weight ratio of hygroscopic plasticizer to non-hygroscopic plasticizer of about 3:1 to about 5:1 and is free of chemically modified gelatin, the composition has a baseline peroxide value not greater than 5 meg/kg and upon storage of the composition at 25.degree. C. and 60% RH for a period of 6 months, the composition has a second peroxide value not greater than 8 meq/kg and if the film-forming material comprises gelatin, the capsule shell has a gelatin:glycerol weight ratio greater than 5:1.

26. The composition of claim 25 wherein the hygroscopic plasticizer comprises glycerol and sorbitol and the non-hygroscopic plasticizer comprises maltitol.

27. The pharmaceutical composition of claim 25 wherein the composition has a baseline peroxide value not greater than 5 meq/kg and upon storage of the composition at 25.degree. C. and 60% RH for a period of 6 months, the composition has a second peroxide value not greater than 5 meg/kg.

28. The pharmaceutical composition of claim 25 wherein the composition has a dissolution profile as measured by rotating dialysis cell method at a paddle speed 100 rpm and a pH 1.2, wherein: (1) at least about 20% of the ethyl eicosapentaenoate is dissolved by 10 minutes; (2) at least about 50% of the ethyl eicosapentaenoate is dissolved by 30 minutes; (3) at least about 80% of the ethyl eicosapentaenoate is dissolved by 60 minutes; or (4) at least about 95% of the ethyl eicosapentaenoate is dissolved by 100 minutes.

29. The pharmaceutical composition of claim 28 wherein the composition has a dissolution profile as measured by rotating dialysis cell method at a paddle speed 100 rpm and a pH 1.2, wherein: (1) at least about 20% of the ethyl eicosapentaenoate is dissolved by 10 minutes; (2) at least about 45% of the ethyl eicosapentaenoate is dissolved by 30 minutes; (3) at least about 80% of the ethyl eicosapentaenoate is dissolved by 60 minutes; and (4) at least about 95% of the ethyl eicosapentaenoate is dissolved by 100 minutes.

30. The pharmaceutical composition of claim 27 wherein upon administration of said composition to a human subject, the subject achieves an eicosapentaenoic acid T.sub.max within 5.8 hours of said administration.

31. The pharmaceutical composition of claim 30 wherein the capsule shell has a gelatin to glycerol ratio of at least 5.2:1.
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